In the present exploration, a sequence of 5’-(substituted aryl)-2-furanyl}-3,4-Dihydro-1H-pyrimidine-2-ones have been designed and synthesized with Beginelli reaction derivatives carried from the reaction of ethyl acetoacetate1, with substituted urea 2 and substituted aryl furfuraldehydes 3 in presence of acetic acid yielded {5’-(substituted aryl)- 2-furanyl}-3,4-Dihydro-1H-pyrimidine-2-ones [4a-k (X=O), 4l-v (X=S)]. All synthesized compounds structures were confirmed by FT-IR, NMR (1H and 13C), Mass spectrometry (MS) and by Elemental analysis. The present exploration also required for in vitro antibacterial activity against Gram positive strains of bacteria, Bacillus cereus (ATCC 11778), Staphylococcus aureus (ATCC 11633), Staphylococcus epidermidis (ATCC 155), Enterococccus faecalis (ATCC 14506) and Gram negative bacterial starins, Shigella dysenteriae (ATCC 13313), Escherichia coli (ATCC11303), Klebsiella pneumoniae (ATCC 10031) and Salmonella typhi (MTCC 733). Tested antimicrobial activity revealed that compounds 4kand 4v showed very promising antibacterial activity and found to be most effective when tested against strains of Klebsiella pneumonia, Staphylococcus aureus, Salmonella typhi, Staphylococcus epidermidis, and Enterococccus faecalis. Although rest synthesized derivatives showed significant antibacterial activity. The novel synthesized compounds also exhibited significant in vitro anti-inflammatory biological activity by utilization of the percent inhibition of protein denaturation method.